Patents Assigned to SmithKline Beckman Corporation
  • Patent number: 4876266
    Abstract: Disclosed are novel substituted 3-aralkylimidazolines of the structure. ##STR1## processes for their preparation, intermediates useful in their preparation, pharmaceutical compositions containing them and their use in therapy in particular as dopamine-.beta.-hydroxylase inhibitors.
    Type: Grant
    Filed: December 31, 1987
    Date of Patent: October 24, 1989
    Assignee: SmithKline Beckman Corporation
    Inventors: Lawrence I. Kruse, Thomas B. Leonard, Stephen T. Ross
  • Patent number: 4876243
    Abstract: Vasopressin-like peptide whose structures have been modified by an alpha-methyl amino acid at the 4 or 7 position are set forth. These compounds have potent vasopressin antagonist activities.
    Type: Grant
    Filed: August 27, 1987
    Date of Patent: October 24, 1989
    Assignee: Smithkline Beckman Corporation
    Inventors: Garland R. Marshall, Michael L. Moore
  • Patent number: 4874792
    Abstract: This invention relates to alkanoic acid compounds having phenyl and thio substituents which are useful as leukotriene antagonists and pharmaceutical compositions containing such compounds. This invention also relates to treating diseases in which leukotrienes are a factor by administration of an effective amount of the above compounds or compositions.
    Type: Grant
    Filed: March 25, 1988
    Date of Patent: October 17, 1989
    Assignee: Smithkline Beckman Corporation
    Inventors: John G. Gleason, Ralph F. Hall, Thomas W. Ku, Carl D. Perchonock
  • Patent number: 4873357
    Abstract: Potent dopamine-.beta.-hydroxylase inhibitors having the Formula: ##STR1## which are useful to inhibit dopamine-.beta.-hydroxylase activity, pharmaceutical compositions including these inhibitors, and methods of using these inhibitors to inhibit dopamine-.beta.-hydroxylase activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented inhibitors.
    Type: Grant
    Filed: October 8, 1987
    Date of Patent: October 10, 1989
    Assignee: SmithKline Beckman Corporation
    Inventors: Carl Kaiser, Lawrence I. Kruse, Stephen T. Ross
  • Patent number: 4871771
    Abstract: A method for inhibiting the effects of LTB.sub.4 comprises administration of an effective amount of a compound represented by the following structural formula (I) ##STR1## wherein m is 1 or 2; n is 1, 2 or 3; p is 0, 1, or 2; R' is hydrogen or methyl; R is phenyl substituted with A, R.sub.1 and R.sub.2 wherein R.sub.1 and R.sub.2 are independently selected from either (1) (S).sub.a --(CH.sub.2).sub.b --(T).sub.c --B wherein a is 0 or 1; b is 5 to 12; c is 0 or 1; S and T are independently sulfur, oxygen, or CH.sub.2 with the proviso that S or T are not sulfur when p is 1 or 2; and B is C.sub.1-4 alkyl, ethynyl, trifluoromethyl, or phenyl optionally monosubstituted with Br, Cl, CF.sub.3, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, methylthio, or trifluoromethylthio; or (2) hydrogen bromo, chloro, methyl, trifluoromethyl, methoxy or nitro; and A is selected from (2) as defined above or a pharmaceutically acceptable salt thereof. Such methods are useful in the treatment of diseases in which LTB.sub.4 is a factor.
    Type: Grant
    Filed: February 4, 1988
    Date of Patent: October 3, 1989
    Assignee: SmithKline Beckman Corporation
    Inventors: John G. Gleason, Sylvia T. Hoffstein, Charles M. Kinzig, Seymour Mong, Henry M. Sarau
  • Patent number: 4865982
    Abstract: A DNA fragment from Streptomyces sp. which contains the XP55 gene expression unit.
    Type: Grant
    Filed: May 29, 1985
    Date of Patent: September 12, 1989
    Assignee: SmithKline Beckman Corporation
    Inventors: William V. Burnett, Jr., Thomas G. Eckhardt, Louis R. Fare
  • Patent number: 4863944
    Abstract: Potent DBH Inhibitors having the formula: ##STR1## wherein R is --CO.sub.2 H or --CH.sub.2 NHR.sup.1 can be used to inhibit DBH activity in mammals.
    Type: Grant
    Filed: June 6, 1988
    Date of Patent: September 5, 1989
    Assignee: SmithKline Beckman Corporation
    Inventors: James S. Frazee, Carl Kaiser
  • Patent number: 4861771
    Abstract: Prodrug carbamate derivatives of fenoldopam which provide fenoldopam plasma levels of similar magnitude and over a much longer period of time than the parent compound. An absence of a high initial peak effect associated with the parent compound is noted. A lead compound of the series is 6-chloro-7,8-diethylcarbamoyl-1-(4'-ethylcarbamoylphenyl)-2,3,4,5-tetrahyd ro-1H-3-benzazepine. The R-enantiomers are the most biologically active and preferred compounds.
    Type: Grant
    Filed: January 27, 1989
    Date of Patent: August 29, 1989
    Assignee: SmithKline Beckman Corporation
    Inventors: Dimitri Gaitanopoulos, Bruce Mico, Joseph Weinstock
  • Patent number: 4859779
    Abstract: Potent dopamine-.beta.-hydroxylase inhibitors having the formula ##STR1## that are useful to inhibit dopamine-.beta.-hydroxylase activity, pharmaceutical compositions including these inhibitors, and methods of using these inhibitors to inhibit dopamine-.beta.-hydroxylase activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented inhibitors.
    Type: Grant
    Filed: January 27, 1989
    Date of Patent: August 22, 1989
    Assignee: SmithKline Beckman Corporation
    Inventors: Joseph A. Finkelstein, Lawrence I. Kruse, Thomas B. Leonard
  • Patent number: 4859584
    Abstract: Methods for determining growth rate of cells growing in vivo and in vitro. Cells are labelled with cyanine dyes and changes in plasma membrane cyanine dye levels are used to determine growth rate. Cell growth rate determinations are utilized to monitor transplanted bone marrow cell engraftment and post-surgical corneal epitheal cell growth. The invented methods also are used to determine tumor cell sensitivity to cancer therapeutic agents, yeast sensitivity to antifungal agents, and bacteria sensitivity to antibacterial agents.
    Type: Grant
    Filed: October 31, 1986
    Date of Patent: August 22, 1989
    Assignee: SmithKline Beckman Corporation
    Inventors: Paul K. Horan, Bruce D. Jensen, Sue E. Slezak
  • Patent number: 4859601
    Abstract: A DNA fragment from Streptomyces sp. which contains the Bgl protein (P49) promoter, the P1 promoter, for expressing heterologous genes.
    Type: Grant
    Filed: January 21, 1986
    Date of Patent: August 22, 1989
    Assignee: SmithKline Beckman Corporation
    Inventors: William V. Burnett, Jr., Thomas G. Eckhardt, Louis R. Fare
  • Patent number: 4857549
    Abstract: Compounds, pharmaceutical compositions and a method for treating tumors by administering an effective tumor cell growth-inhibiting amount of a .alpha.,.omega.-bis(disubstitutedphosphino)hydrocarbon compound or a [.alpha.,.omega.-bis(disubstitutedphosphino)hydrocarbon] digold(I), digold(III, disiliver(I) or dicopper(I) complex to an animal afflicted by such tumor cells.
    Type: Grant
    Filed: February 26, 1988
    Date of Patent: August 15, 1989
    Assignee: SmithKline Beckman Corporation
    Inventors: David T. Hill, Randall K. Johnson, Christopher K. Mirabelli
  • Patent number: 4857540
    Abstract: 1-substituted-2-mercapto(or aminomethyl)benzimidazole compounds which inhibit dopamine-.beta.-hydroxylase activity.
    Type: Grant
    Filed: November 27, 1987
    Date of Patent: August 15, 1989
    Assignee: SmithKline Beckman Corporation
    Inventors: Carl Kaiser, Lawrence I. Kruse
  • Patent number: 4849362
    Abstract: Invented are new tetracarboxylate compounds which are chelators for calcium ions. Also invented is a useful method of measuring intracellular calcium concentrations using these novel compounds as an optical indicator.
    Type: Grant
    Filed: May 19, 1988
    Date of Patent: July 18, 1989
    Assignee: SmithKline Beckman Corporation
    Inventors: Robert M. DeMarinis, Haralambos E. Katerinopoulos, Katharine A. Muirhead
  • Patent number: 4847270
    Abstract: Novel compounds, pharmaceutical compositions and a method of inhibiting the 5-lipoxygenase products in an animal in need thereof which comprises administering an effective, 5-lipoxygenase pathway inhibiting amount of a 2,2'-[1,2-ethanediylbis-(thio)]-bis-1H-imidazole or 2,2'-[1,3-propan-2-onediylbis-(thio)]bis-1H-imidazole, or a pharmaceutically acceptable salt thereof, to such animal.
    Type: Grant
    Filed: November 10, 1987
    Date of Patent: July 11, 1989
    Assignee: SmithKline Beckman Corporation
    Inventors: Paul E. Bender, David T. Hill
  • Patent number: 4843163
    Abstract: 3-(2-Phenethyl)-1-carbamoyloxypyridinium halide is an intermediate for the preparation of the antihistamine azatadine.
    Type: Grant
    Filed: December 2, 1987
    Date of Patent: June 27, 1989
    Assignee: SmithKline Beckman Corporation
    Inventors: Raymond E. Dagger, Linda A. Motyka
  • Patent number: 4840892
    Abstract: Polynucleotide hybridization probes are labeled in non-probe regions but not in probe regions by selectively protecting probe regions prior to modification of the polynucleotide.
    Type: Grant
    Filed: April 15, 1985
    Date of Patent: June 20, 1989
    Assignee: Smithkline Beckman Corporation
    Inventors: Craig W. Adams, Jeffry J. Leary, Martin Rosenberg
  • Patent number: 4839371
    Abstract: Disclosed are novel substituted 3-aralkyl-2-mercaptopyridines of the structure: ##STR1## processes for their preparation, intermediates useful in their preparation, pharmaceutical compositions containing them and their use in therapy in particular as dopamine-.beta.-hydroxylase inhibitors.
    Type: Grant
    Filed: September 17, 1987
    Date of Patent: June 13, 1989
    Assignee: SmithKline Beckman Corporation
    Inventors: Lawrence I. Kruse, Stephen T. Ross
  • Patent number: 4837353
    Abstract: 2-(N-Phenylakyl-N-formyl)amino-3-hydroxy-2-propenoic acids are intermediates for mercaptoimidazolecarboxylic acids which are dopamine-.beta.-hydroxylase inhibitors.
    Type: Grant
    Filed: January 21, 1988
    Date of Patent: June 6, 1989
    Assignee: SmithKline Beckman Corporation
    Inventors: Joseph A. Finkelstein, Lawrence I. Kruse, Thomas B. Leonard
  • Patent number: 4835154
    Abstract: Potent dopamine-.beta.-hydroxylase inhibitors having the Formula ##STR1## that are useful to inhibit dopamine-.beta.-hydroxylase activity, pharmaceutical compositions including these inhibitors, and methods of using these inhibitors to inhibit dopamine-.beta.-hydroxylase activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented inhibitors.
    Type: Grant
    Filed: June 1, 1987
    Date of Patent: May 30, 1989
    Assignee: SmithKline Beckman Corporation
    Inventors: Joseph A. Finkelstein, Lawrence I. Kruse